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CA2367130A1 - Composes 6-azaindole utilises comme antagonistes d'une hormone liberant la gonadotropine - Google Patents

Composes 6-azaindole utilises comme antagonistes d'une hormone liberant la gonadotropine Download PDF

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Publication number
CA2367130A1
CA2367130A1 CA002367130A CA2367130A CA2367130A1 CA 2367130 A1 CA2367130 A1 CA 2367130A1 CA 002367130 A CA002367130 A CA 002367130A CA 2367130 A CA2367130 A CA 2367130A CA 2367130 A1 CA2367130 A1 CA 2367130A1
Authority
CA
Canada
Prior art keywords
substituted
alkyl
aryl
compound
aralkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA002367130A
Other languages
English (en)
Inventor
Thomas F. Walsh
Feroze Ujjainwalla
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2367130A1 publication Critical patent/CA2367130A1/fr
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Cette invention concerne des composés de formule (I) et des sels de ces composés acceptables au plan pharmaceutiques qui jouent un rôle utile en tant qu'antagonistes de GnRH et qui, en tant que tels, peuvent convenir pour le traitement de diverses pathologies en rapport avec diverses hormones sexuelles et autres pathologies connexes, tant chez l'homme que chez la femme.
CA002367130A 1999-03-10 2000-03-06 Composes 6-azaindole utilises comme antagonistes d'une hormone liberant la gonadotropine Abandoned CA2367130A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12361699P 1999-03-10 1999-03-10
US60/123,616 1999-03-10
PCT/US2000/005836 WO2000053185A1 (fr) 1999-03-10 2000-03-06 Composes 6-azaindole utilises comme antagonistes d'une hormone liberant la gonadotropine

Publications (1)

Publication Number Publication Date
CA2367130A1 true CA2367130A1 (fr) 2000-09-14

Family

ID=22409746

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002367130A Abandoned CA2367130A1 (fr) 1999-03-10 2000-03-06 Composes 6-azaindole utilises comme antagonistes d'une hormone liberant la gonadotropine

Country Status (6)

Country Link
US (1) US6288078B1 (fr)
EP (1) EP1171135A4 (fr)
JP (1) JP2002538208A (fr)
AU (1) AU3514200A (fr)
CA (1) CA2367130A1 (fr)
WO (1) WO2000053185A1 (fr)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0022670D0 (en) 2000-09-15 2000-11-01 Astrazeneca Ab Molecules
SE0100568D0 (sv) * 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
SE0100566D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
SE0101692D0 (sv) 2001-05-14 2001-05-14 Astrazeneca Ab Compounds
TW200407127A (en) 2002-08-21 2004-05-16 Astrazeneca Ab Chemical compounds
US7253290B2 (en) 2002-08-21 2007-08-07 Astrazeneca Ab Pyrazole derivatives as GnRH inhibitors
DE60318716T2 (de) * 2002-08-21 2009-01-08 Astrazeneca Ab Thieno-pyrrole verbindungen als antagonisten der gonadotropin-freisetzenden hormonrezeptoren
TW200413351A (en) 2002-08-21 2004-08-01 Astrazeneca Ab Chemical compounds
GB0219472D0 (en) 2002-08-21 2002-10-02 Astrazeneca Ab Chemical compounds
OA13050A (en) 2003-04-29 2006-11-10 Pfizer Ltd 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension.
GB0327323D0 (en) * 2003-11-24 2003-12-31 Pfizer Ltd Novel pharmaceuticals
US7572799B2 (en) * 2003-11-24 2009-08-11 Pfizer Inc Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors
WO2005079805A1 (fr) * 2004-02-20 2005-09-01 Astrazeneca Ab Derives de pyrrole utilises en tant qu'antagonistes de l'hormone liberant de la gonadotrophine (gnrh)
CA2562251C (fr) 2004-04-07 2009-04-28 Pfizer Inc. Pyrazolo'4,3-d pyrimidines
PL1753764T3 (pl) 2004-06-09 2009-04-30 Glaxo Group Ltd Pochodne pirolopirydyny
US7601725B2 (en) 2004-07-16 2009-10-13 Sunesis Pharmaceuticals, Inc. Thienopyrimidines useful as Aurora kinase inhibitors
US7932257B2 (en) 2005-07-22 2011-04-26 Sunesis Pharmaceuticals, Inc. Substituted pyrazolo[4,3-d]pyrimidines as aurora kinase inhibitors
AR067354A1 (es) * 2007-06-29 2009-10-07 Sunesis Pharmaceuticals Inc Compuestos utiles como inhibidores de la raf quinasa
NZ582349A (en) * 2007-06-29 2012-06-29 Sunesis Pharmaceuticals Inc Heterocyclic compounds useful as raf kinase inhibitors
CN101903381A (zh) * 2007-10-24 2010-12-01 日本医事物理股份有限公司 对淀粉样蛋白具有亲和性的新化合物
US20100061976A1 (en) * 2008-07-24 2010-03-11 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Method for treating or preventing osteoporosis by reducing follicle stimulating hormone to cyclic physiological levels in a mammalian subject
WO2018002673A1 (fr) 2016-07-01 2018-01-04 N4 Pharma Uk Limited Nouvelles formulations d'antagonistes du récepteur de l'angiotensine ii

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2181559A1 (en) 1972-04-28 1973-12-07 Aec Chimie Organique Bio N-Phenylalkyl-N-3-indolylalkyl-alkylamines - with sedative, neuroleptic, analgesic, hypotensive, antiserotonin, adrenolytic activity
ZA795239B (en) 1978-10-12 1980-11-26 Glaxo Group Ltd Heterocyclic compounds
US4544663A (en) 1984-05-07 1985-10-01 Sandoz, Inc. Indolamine derivatives as anti-fertility agents
WO1990005721A1 (fr) 1988-11-14 1990-05-31 The Upjohn Company Acides alpha-amino-indole-3-acetiques utiles en tant qu'agents anti-diabetiques, anti-obesite et anti-athero-sclerotiques
US5030640A (en) 1989-01-05 1991-07-09 Merck & Co., Inc. Novel β-adrenergic agonists and pharmaceutical compositions thereof
TW449600B (en) * 1994-04-19 2001-08-11 Takeda Chemical Industries Ltd Condensed-ring thiophene derivatives, their production and use
US5607939A (en) 1994-04-28 1997-03-04 Takeda Chemical Industries, Ltd. Condensed heterocyclic compounds, their production and use
DE69528257T2 (de) 1994-04-29 2003-05-15 Takeda Chemical Industries, Ltd. KONDENSIERTE HETEROCYCLISCHE VERBINDUNG, DEREN HERSTELLUNG UND VERWENDUNG ALS GnRH ANTAGONISTEN
GB2298199A (en) * 1995-02-21 1996-08-28 Merck Sharp & Dohme Synthesis of azaindoles
US5780437A (en) 1995-12-14 1998-07-14 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US5849764A (en) * 1995-12-14 1998-12-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
EA000828B1 (ru) 1995-12-14 2000-04-24 Мерк Энд Ко., Инк. Антагонисты гонадотропин-высвобождающего фактора
US5756507A (en) 1995-12-14 1998-05-26 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU709090B2 (en) 1995-12-14 1999-08-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
EP1161431A4 (fr) * 1999-03-10 2002-04-24 Merck & Co Inc Composes 6-azaindole utilises comme antagonistes d'une hormone liberant la gonadotropine

Also Published As

Publication number Publication date
AU3514200A (en) 2000-09-28
US6288078B1 (en) 2001-09-11
EP1171135A1 (fr) 2002-01-16
WO2000053185A1 (fr) 2000-09-14
JP2002538208A (ja) 2002-11-12
EP1171135A4 (fr) 2002-05-15

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Legal Events

Date Code Title Description
FZDE Discontinued